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所有产品(19) Rho抑制剂(18) Rho激活剂(1)

目录号	产品描述	文献引用	实验数据
S1573	Fasudil (HA-1077) HCl Fasudil (HA-1077, AT-877)是一种有效的、具有选择性的Rho抑制剂（ROCK2, Ki=0.33 μM），同时对PKA、PKG、PKC和MLCK也具有抑制活性，Ki值分别为1.6 μM、1.6 μM、3.3 μM、36 μM。Fasudil 也是calcium channel的阻滞剂。	Proc Natl Acad Sci U S A, 2021, 118(2)e2016034118 J Neurochem, 2021, 10.1111/jnc.15436 Cell Regen, 2021, 10(1):8	The ROCK inhibitors fasudil and Y27632 prevented SCP2 cell bone metastasis in nude mice (n = 10 per group). Shown are BLI images of bone metastases, IHC analyses of SMAD3 C-tail phosphorylation and PTHLH, osteoclast TRAP staining, and BLI quantitation.
S1314	Zoledronic acid (ZOL 446) Zoledronic acid (ZOL 446, ZA, Zoledronate, CGP-4244, GP42446A, Zometa, Zomera, Aclasta, Reclast), 破骨细胞抑制剂，通过抑制甲羟戊酸途径诱导破骨细胞凋亡，并防止小GTP结合蛋白，如Ras 和 Rho的异戊二烯化。Zoledronic acid (ZA) 还可诱导自噬。	Biomater Sci, 2021, 10.1039/d0bm02107e Hum Cell, 2021, 10.1007/s13577-021-00579-z Aging Cell, 2020, 29	Isolation of cd T cells. PBMCs were cultured in the presence of 400 nM ZA and 200 IU/ml IL-2 over 10 days. cd T cells were isolated by negative MACS isolation. Flow cytometric analysis revealed co-expression of CD3 and TCRcd on over 99% of cells of the flow through fraction (A). The T cells expressed the TCRVd2 chain (B) and the CD56 protein (C).
S8031	NSC 23766 NSC 23766是一种Rac GTPase抑制剂，通过鸟嘌呤核苷酸因子(GEFs)靶向作用于Rac 活化，无细胞试验中IC50为~50 μM；但是不会抑制密切相关的靶点，Cdc42或RhoA。	Theranostics, 2021, 11(9):4316-4334 Elife, 2021, 10e65962 BMC Biol, 2021, 19(1):140	MES cells were treated with Rac inhibitor (50 μM EHT1864 or NSC23766) and assayed for self-renewal by serial passage mammosphere formation. P1, passage 1; P2, passage 2. Data are means ± SEM of three biological replicates. *P ≤ 0.05 by two-tailed t test.
S7319	EHop-016 EHop-016 是一种特异性Rac GTPase抑制剂，在MDA-MB-435 和 MDA-MB-231细胞中作用于Rac1，IC50为1.1 μM，同等有效抑制Rac3。	PLoS Biol, 2021, 19(4):e3001134 PLoS Genet, 2020, 16(3):e1008694 Stem Cell Res Ther, 2020, 11(1):525	(f) Liver samples from both groups treated with olive oil, CCl4, CCl4+NSC23766 or +EHop-016 for 4 weeks were collected for Rac1 activity assay and western blot analysis.
S1721	Azathioprine Azathioprine 是一种抑制免疫系统的药物，抑制了嘌呤的合成以及GTP结合蛋白Rac1的激活，用于器官移植和自身免疫性疾病。	Sci Rep, 2019, 9(1):4360 Blood, 2016, 1;128(9):1234-45
S6875^New	CASIN CASIN (Pirl1-related Compound 2) 可直接抑制 Cdc42/RhoGDI 的激活，其IC50值为2 μM。
S6000^New	CID44216842 CID44216842 (Cdc42-IN-1)是一种有效的 Cdc42 选择性鸟嘌呤核苷酸结合先导抑制剂，在 GTP 结合测定中对 Cdc42^WT 和 Cdc42^Q61L 的 EC50 分别为 1.0 μM 和 1.2 μM。
S7293	ZCL278 ZCL278是一个选择性的Cdc42 GTP酶抑制剂，Kd为11.4 μM。	Front Oncol, 2021, 11:656608 EBioMedicine, 2019, 50:122-134 J Bone Miner Res, 2018, 33(5):945-958	Rho GTPases were involved in NaAsO2 induced apoptosis in rat CGNs. A. Representative fluorescence images of cells exposed to 0 and 10 μM NaAsO2 for 24 h with or without ZCL278 (an inhibitor of Cdc42), or a Rac1 inhibitor NSC23766. Both ZCL278 and NSC23766 reduced the apoptotic cells. B. The graph indicates TUNEL-positive rat CGNs exposed to NaAsO2 (10 μM) with ZCL278 or NSC23766 groups decreased significantly compared with those of NaAsO2 treatment group. Data are expressed as mean ± SD from at least 5 visual fields. C. Rat CGNs in 96-well plates were treated by 0 and 10 μM NaAsO2 for 24h with or without ZCL278 (an inhibitor of Cdc42) pretreatment for 1 h, or a Rac1 inhibitor NSC23766 pretreatment for 12 h, and assessed by a CCK-8. ZCL278 and NSC23766 increased rat CGNs viability exposed to NaAsO2. All statistical results are expressed as means±SD from at least three independent experiments. ***P<0.001 vs control, # P<0.05, ##P<0.01, ###P<0.001 VS NaAsO2 treatment group.
S8749	MBQ-167 MBQ-167是一种有效的Rac和Cdc42双重抑制剂，在转移性乳腺癌细胞中，IC50分别为103 nM和78 nM。	Mol Cancer, 2021, 20(1):77 Cell, 2020, 182(3):685-712.e19 Cell, 2020, 182(3):685-712.e19
S7719	CCG-1423 CCG-1423是一种特定的 RhoA 通路抑制剂，能够抑制SRF介导的转录。	Front Cell Dev Biol, 2021, 9:664375 Front Cell Dev Biol, 2021, 9:583492 Microb Pathog, 2021, 158:105054	Cells were treated with CCG-1423 for 48 h. CCG-1423 blocked the nuclear translocation of MRTF-A.
S8469	CCG-203971 CCG-203971是一种新型的Rho/MRTF/SRF通路抑制剂，对SRE.L.的IC50值为0.64 μM。它可以抑制Rho介导的基因转录。	J Cell Physiol, 2020, 235(5):4790-4803 Small GTPases, 2020, 10.1080/21541248
S6673	CCG-222740 CCG-222740是一种Rho/MRTF通路抑制剂。CCG-222740通过降低α平滑肌肌动蛋白(alpha smooth muscle actin, α-SMA)的表达水平来降低星状细胞在体外和体内的活化。
S8988	Rhosin hydrochloride Rhosin (G04) hydrochloride (HCl) 是RhoA亚家族 Rho GTPases 的强效特异性抑制剂，Kd值约为0.4 uM。Rhosin hydrochloride 可诱导细胞凋亡。
S7482	EHT 1864 2HCl EHT 1864 2HCl是一种强效的Rac family GTPase抑制剂，其对Rac1, Rac1b, Rac2 和 Rac3的K_d分别为40 nM, 50 nM, 60 nM 和 250 nM 。	J Appl Toxicol, 2021, 10.1002/jat.4175 Cell, 2020, 182(3):685-712.e19 Cell, 2020, 182(3):685-712.e19	E) Representative images of 3-dimensional visualization of vessel networks, H&E staining, and Masson staining. Dotted straight line indicates the femur—implant junction (F, femur; I, implant). Black box, implant region; blue arrows, osteocytes; yellow arrows, osteoblast cells; black triangle, newly formed bone or implant debris, black arrows, chondrocyte-like cells; red triangle, blood sinus. Scale bars, 200 μm.
S7686	ML141 ML141 (CID-2950007) 是 Rho 家族GTPase cdc42的一种有效的，选择性可逆非竞争性抑制剂，IC50为200 nM。对cdc42比对其他Rho家族中的GTPases(如Rac1, Rab2, Rab7)更有选择性。 ML141 与 p38 激活增加有关，并可能诱导p38依赖性凋亡/衰老。ML141还可保护神经母细胞瘤细胞免受二甲双胍(metformin)诱导的凋亡。	Cell Rep, 2021, 36(1):109254 FASEB J, 2021, 35(5):e21598 Sci Rep, 2021, 11(1):8168	(A) The survival rate detected at 72 h after the injection of different concentrations of ML141; shrimp injected with DMSO were used as controls. (B) The expression of WSSV IE1 at the mRNA level at 24 h post ML141 injection. Shrimp injected with the same amount of DMSO in each group were used as controls.
S0890	MLS000532223 MLS000532223 是一种 Rho family GTPases 的高亲和力的选择性抑制剂，EC50值为16 μM至120 μM。
S5244	Zoledronic acid monohydrate Zoledronic acid (Zoledronate, CGP-4244) monohydrate 是 Zoledronic acid (唑来膦酸) 的一水合物，是有效的破骨细胞抑制剂，可通过抑制甲戊二羟酸途径的酶、阻止小GTP结合蛋白如Ras和Rho的异戊二烯化来诱导破骨细胞凋亡。	Biomater Sci, 2021, 10.1039/d0bm02107e Cancers (Basel), 2020, 31;12(1) pii: E104 J Cell Mol Med, 2020, 25
S6752	Y16 Y16是G蛋白偶联Rho GEFs抑制剂。它能阻止LARG和Rho的结合，Kd值为80 nM。
S0765	MAZ51 MAZ51 是一种选择性的 vascular endothelial growth factor receptor (VEGFR)-3 (Flt-4) tyrosine kinase 的有效抑制剂。MAZ51 通过 Akt/GSK3β 的磷酸化和 RhoA 的激活来诱导神经胶质瘤细胞的细胞圆缩和G2/M细胞周期停滞。 MAZ51 可抑制多种非VEGFR-3表达肿瘤细胞的增殖并诱导其凋亡。

目录号	产品描述	文献引用	实验数据
S1573	Fasudil (HA-1077) HCl Fasudil (HA-1077, AT-877)是一种有效的、具有选择性的Rho抑制剂（ROCK2, Ki=0.33 μM），同时对PKA、PKG、PKC和MLCK也具有抑制活性，Ki值分别为1.6 μM、1.6 μM、3.3 μM、36 μM。Fasudil 也是calcium channel的阻滞剂。	Proc Natl Acad Sci U S A,2021, 118(2)e2016034118 J Neurochem,2021, 10.1111/jnc.15436 Cell Regen,2021, 10(1):8	The ROCK inhibitors fasudil and Y27632 prevented SCP2 cell bone metastasis in nude mice (n = 10 per group). Shown are BLI images of bone metastases, IHC analyses of SMAD3 C-tail phosphorylation and PTHLH, osteoclast TRAP staining, and BLI quantitation.
S1314	Zoledronic acid (ZOL 446) Zoledronic acid (ZOL 446, ZA, Zoledronate, CGP-4244, GP42446A, Zometa, Zomera, Aclasta, Reclast), 破骨细胞抑制剂，通过抑制甲羟戊酸途径诱导破骨细胞凋亡，并防止小GTP结合蛋白，如Ras 和 Rho的异戊二烯化。Zoledronic acid (ZA) 还可诱导自噬。	Biomater Sci,2021, 10.1039/d0bm02107e Hum Cell,2021, 10.1007/s13577-021-00579-z Aging Cell,2020, 29	Isolation of cd T cells. PBMCs were cultured in the presence of 400 nM ZA and 200 IU/ml IL-2 over 10 days. cd T cells were isolated by negative MACS isolation. Flow cytometric analysis revealed co-expression of CD3 and TCRcd on over 99% of cells of the flow through fraction (A). The T cells expressed the TCRVd2 chain (B) and the CD56 protein (C).
S8031	NSC 23766 NSC 23766是一种Rac GTPase抑制剂，通过鸟嘌呤核苷酸因子(GEFs)靶向作用于Rac 活化，无细胞试验中IC50为~50 μM；但是不会抑制密切相关的靶点，Cdc42或RhoA。	Theranostics,2021, 11(9):4316-4334 Elife,2021, 10e65962 BMC Biol,2021, 19(1):140	MES cells were treated with Rac inhibitor (50 μM EHT1864 or NSC23766) and assayed for self-renewal by serial passage mammosphere formation. P1, passage 1; P2, passage 2. Data are means ± SEM of three biological replicates. *P ≤ 0.05 by two-tailed t test.
S7319	EHop-016 EHop-016 是一种特异性Rac GTPase抑制剂，在MDA-MB-435 和 MDA-MB-231细胞中作用于Rac1，IC50为1.1 μM，同等有效抑制Rac3。	PLoS Biol,2021, 19(4):e3001134 PLoS Genet,2020, 16(3):e1008694 Stem Cell Res Ther,2020, 11(1):525	(f) Liver samples from both groups treated with olive oil, CCl4, CCl4+NSC23766 or +EHop-016 for 4 weeks were collected for Rac1 activity assay and western blot analysis.
S1721	Azathioprine Azathioprine 是一种抑制免疫系统的药物，抑制了嘌呤的合成以及GTP结合蛋白Rac1的激活，用于器官移植和自身免疫性疾病。	Sci Rep,2019, 9(1):4360 Blood,2016, 1;128(9):1234-45
S6875^New	CASIN CASIN (Pirl1-related Compound 2) 可直接抑制 Cdc42/RhoGDI 的激活，其IC50值为2 μM。
S6000^New	CID44216842 CID44216842 (Cdc42-IN-1)是一种有效的 Cdc42 选择性鸟嘌呤核苷酸结合先导抑制剂，在 GTP 结合测定中对 Cdc42^WT 和 Cdc42^Q61L 的 EC50 分别为 1.0 μM 和 1.2 μM。
S7293	ZCL278 ZCL278是一个选择性的Cdc42 GTP酶抑制剂，Kd为11.4 μM。	Front Oncol,2021, 11:656608 EBioMedicine,2019, 50:122-134 J Bone Miner Res,2018, 33(5):945-958	Rho GTPases were involved in NaAsO2 induced apoptosis in rat CGNs. A. Representative fluorescence images of cells exposed to 0 and 10 μM NaAsO2 for 24 h with or without ZCL278 (an inhibitor of Cdc42), or a Rac1 inhibitor NSC23766. Both ZCL278 and NSC23766 reduced the apoptotic cells. B. The graph indicates TUNEL-positive rat CGNs exposed to NaAsO2 (10 μM) with ZCL278 or NSC23766 groups decreased significantly compared with those of NaAsO2 treatment group. Data are expressed as mean ± SD from at least 5 visual fields. C. Rat CGNs in 96-well plates were treated by 0 and 10 μM NaAsO2 for 24h with or without ZCL278 (an inhibitor of Cdc42) pretreatment for 1 h, or a Rac1 inhibitor NSC23766 pretreatment for 12 h, and assessed by a CCK-8. ZCL278 and NSC23766 increased rat CGNs viability exposed to NaAsO2. All statistical results are expressed as means±SD from at least three independent experiments. ***P<0.001 vs control, # P<0.05, ##P<0.01, ###P<0.001 VS NaAsO2 treatment group.
S8749	MBQ-167 MBQ-167是一种有效的Rac和Cdc42双重抑制剂，在转移性乳腺癌细胞中，IC50分别为103 nM和78 nM。	Mol Cancer,2021, 20(1):77 Cell,2020, 182(3):685-712.e19 Cell,2020, 182(3):685-712.e19
S7719	CCG-1423 CCG-1423是一种特定的 RhoA 通路抑制剂，能够抑制SRF介导的转录。	Front Cell Dev Biol,2021, 9:664375 Front Cell Dev Biol,2021, 9:583492 Microb Pathog,2021, 158:105054	Cells were treated with CCG-1423 for 48 h. CCG-1423 blocked the nuclear translocation of MRTF-A.
S8469	CCG-203971 CCG-203971是一种新型的Rho/MRTF/SRF通路抑制剂，对SRE.L.的IC50值为0.64 μM。它可以抑制Rho介导的基因转录。	J Cell Physiol,2020, 235(5):4790-4803 Small GTPases,2020, 10.1080/21541248
S6673	CCG-222740 CCG-222740是一种Rho/MRTF通路抑制剂。CCG-222740通过降低α平滑肌肌动蛋白(alpha smooth muscle actin, α-SMA)的表达水平来降低星状细胞在体外和体内的活化。
S8988	Rhosin hydrochloride Rhosin (G04) hydrochloride (HCl) 是RhoA亚家族 Rho GTPases 的强效特异性抑制剂，Kd值约为0.4 uM。Rhosin hydrochloride 可诱导细胞凋亡。
S7482	EHT 1864 2HCl EHT 1864 2HCl是一种强效的Rac family GTPase抑制剂，其对Rac1, Rac1b, Rac2 和 Rac3的K_d分别为40 nM, 50 nM, 60 nM 和 250 nM 。	J Appl Toxicol,2021, 10.1002/jat.4175 Cell,2020, 182(3):685-712.e19 Cell,2020, 182(3):685-712.e19	E) Representative images of 3-dimensional visualization of vessel networks, H&E staining, and Masson staining. Dotted straight line indicates the femur—implant junction (F, femur; I, implant). Black box, implant region; blue arrows, osteocytes; yellow arrows, osteoblast cells; black triangle, newly formed bone or implant debris, black arrows, chondrocyte-like cells; red triangle, blood sinus. Scale bars, 200 μm.
S7686	ML141 ML141 (CID-2950007) 是 Rho 家族GTPase cdc42的一种有效的，选择性可逆非竞争性抑制剂，IC50为200 nM。对cdc42比对其他Rho家族中的GTPases(如Rac1, Rab2, Rab7)更有选择性。 ML141 与 p38 激活增加有关，并可能诱导p38依赖性凋亡/衰老。ML141还可保护神经母细胞瘤细胞免受二甲双胍(metformin)诱导的凋亡。	Cell Rep,2021, 36(1):109254 FASEB J,2021, 35(5):e21598 Sci Rep,2021, 11(1):8168	(A) The survival rate detected at 72 h after the injection of different concentrations of ML141; shrimp injected with DMSO were used as controls. (B) The expression of WSSV IE1 at the mRNA level at 24 h post ML141 injection. Shrimp injected with the same amount of DMSO in each group were used as controls.
S0890	MLS000532223 MLS000532223 是一种 Rho family GTPases 的高亲和力的选择性抑制剂，EC50值为16 μM至120 μM。
S5244	Zoledronic acid monohydrate Zoledronic acid (Zoledronate, CGP-4244) monohydrate 是 Zoledronic acid (唑来膦酸) 的一水合物，是有效的破骨细胞抑制剂，可通过抑制甲戊二羟酸途径的酶、阻止小GTP结合蛋白如Ras和Rho的异戊二烯化来诱导破骨细胞凋亡。	Biomater Sci,2021, 10.1039/d0bm02107e Cancers (Basel),2020, 31;12(1) pii: E104 J Cell Mol Med,2020, 25
S6752	Y16 Y16是G蛋白偶联Rho GEFs抑制剂。它能阻止LARG和Rho的结合，Kd值为80 nM。

目录号	产品描述	文献引用	实验数据
S0765	MAZ51 MAZ51 是一种选择性的 vascular endothelial growth factor receptor (VEGFR)-3 (Flt-4) tyrosine kinase 的有效抑制剂。MAZ51 通过 Akt/GSK3β 的磷酸化和 RhoA 的激活来诱导神经胶质瘤细胞的细胞圆缩和G2/M细胞周期停滞。 MAZ51 可抑制多种非VEGFR-3表达肿瘤细胞的增殖并诱导其凋亡。

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S0765

MAZ51

MAZ51 是一种选择性的 vascular endothelial growth factor receptor (VEGFR)-3 (Flt-4) tyrosine kinase 的有效抑制剂。MAZ51 通过 Akt/GSK3β 的磷酸化和 RhoA 的激活来诱导神经胶质瘤细胞的细胞圆缩和G2/M细胞周期停滞。 MAZ51 可抑制多种非VEGFR-3表达肿瘤细胞的增殖并诱导其凋亡。

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